Anticandidal, antibacterial, cytotoxic and antioxidant activities of Calendula arvensis flowers.

Calendula arvensis (CA) is one of the important plants used in traditional medicine in Morocco, due to its interesting chemical composition. The present study aimed to determine the anticandidal, antioxidant and antibacterial activities, and the effects of extracts of CA flowers on the growth of myeloid cancer cells. Also, to characterize the chemical composition of the plant. Flowers of CA were collected based on ethnopharmacological information from the villages around the region Rabat-Khemisset, Moroccco. The hexane and methanol extracts were obtained by soxhlet extraction, while aqueous extracts was obtained by maceration in cold water. CA extracts were assessed for antioxidant activity using four different methods (DPPH, FRAP, TEAC, ß-carotene bleaching test). Furthermore, the phenolic and flavonoid contents were measured, also the antimicrobial activity has been evaluated by the well diffusion method using several bacterial and fungal strains. Finally, extracts cytotoxicity was assessed using MTT test. Phytochemical quantification of the methanolic and aqueous extracts revealed that they were rich with flavonoid and phenolic content and were found to possess considerable antioxidant activities. MIC values of methanolic extracts were 12.5-25µg/mL. While MIC values of hexanolic extracts were between 6.25-12.5µg/mL and were bacteriostatic for all bacteria while methanolic and aqueous extracts were bactericidal. In addition, the extracts exhibited no activity on Candida species except the methanolic extract, which showed antifungal activity onCandida tropicalis 1 and Candida famata 1. The methanolic and aqueous extracts also exhibited antimyeloid cancer activity (IC50 of 31µg/mL). In our study, we conclude that the methanolic and aqueous extracts were a promising source of antioxidant, antimicrobial and cytotoxic agents.

Crystal structure of (Z)-ethyl 2-{5-[(2-benzyl-idene-3-oxo-2,3-di-hydro-benzo[b][1,4]thia-zin-4-yl)meth-yl]-1H-1,2,3-triazol-1-yl}acetate.

The title compound, C22H20N4O3S, features two fused six-membered rings linked to a 1,2,3-triazole ring which is attached to an ethyl acetate group. The heterocycle in the benzo-thia-zine residue has an envelope conformation with the S atom being the flap. The conformation of the ethyl acetate side chain, which is directed to the same side of the mol-ecule as the C6 ring of the fused-ring system, may be partially established by a pair of weak intra-molecular C-H⋯O(carbon-yl) inter-actions. The three-dimensional packing is aided by inter-molecular C-H⋯O and C-H⋯N inter-actions.

Crystal structure of 4-benzyl-2H-benzo[b][1,4]thia-zin-3(4H)-one.

In the title compound, C15H13NOS, the thia-zine ring adopts a twisted boat conformation and the dihedral angle between the aromatic rings is 86.54 (4)°. In the crystal, mol-ecules are linked by weak C-H⋯O inter-actions, resulting in chains along [010].

2-Methyl-3-(n-octylsulfan-yl)quinoxaline.

All the non-H atoms of the title compound, C(17)H(24)N(2)S, lie almost in a common plane (r.m.s. deviation = 0.049 Å). The octyl chain adopts an all-trans conformation.

3-Methyl-1-(prop-2-en-1-yl)quinoxalin-2(1H)-one.

In the mol-ecule of the title compound, C(12)H(12)N(2)O, the quinoxaline ring is planar with an r.m.s. deviation of 0.007 (15) Å. The dihedral angle between the quinoxaline and propenyl planes is 82.1 (2)°. The crystal packing is stabilized by offset π-π stacking between the quinoxaline rings [centroid-centroid distance = 3.8832 (9) Å].

1-Benzyl-3-methyl-quinoxalin-2(1H)-one.

The asymmetric unit of the title compound, C(16)H(14)N(2)O, contains three independent mol-ecules. The dihedral angles between the quinoxaline and phenyl planes in the three mol-ecules are 82.58 (8), 85.66 (9) and 85.36 (9)°. The crystal packing is stabilized by C-H⋯O and C-H⋯N hydrogen bonds.

Spectroscopic characterization and theoretical simulation of 1,4-diallylquinoxaline-2,3-dione self dimer.

Room temperature UV-vis absorption and emission spectra of the 1,4-diallylquinoxaline-2,3-dione (DAQX) are measured in solution at different concentrations. Even at very low concentration (approximately 10(-7)M), DAQX is shown to form ground state van der Waals dimers and excited dimers. These later species do not seem to rearrange into an excimer geometry. The theoretical simulation of the dimer, performed using the analytical atom-atom pair potential described below, predicts a non sandwich face-to-reverse slipped structure with head-to-tail orientation. The allowed absorption transitions, calculated using ZINDO/S package, reproduce satisfactory the experimental spectrum for both the monomer and the simulated dimer.

[Synthesis and pharmacological study of three 1-alkyl-3-(ethoxycarbonylmethylene)-2-oxo quinoxalines]. / Synthèse et étude pharmacologique de trois dérivés alkylés de la 3-(éthoxycarbonylméthylène)- 2-oxo quinoxaline.

The acute toxicity study and the psychotropic activity of three alkylated derivatives of 3-(ethoxycarbonylmethylene) -2-oxo quinoxaline did not demonstrate any toxicity of these products at therapeutic dosages. In the animal, these compounds have sedative, myorelaxant and anxiolytic properities.

[Synthesis and pharmacological study of 7-phenyl-1,4-diazepin-5-one and its derivatives]. / Synthèse et étude pharmacologique de dérivés de la 1,4-diazépin-5-one.

We studied the synthesis and psychotropic activity of the 7-phenyl-1,4-diazepin-5-one and derivatives. It can be conclude that these products have sedative, myorelaxant and anxiolytic actions. The toxicity study demonstrated that two diazepines are non-toxic at therapeutic dosages but that a third compound is very toxic.

A new flavonoid from the aerial parts of Chrysanthemum viscidehirtum.

From the aerial parts of Chrysanthemum viscidehirtum, a new flavonoid, 2"-glucosyl-8-C-glucosyl-4'-O-methylapigenin (1) was isolated.

[Synthesis of carbamoyl tetrahydro 1,4,2-dioxazines and evaluation of their activity against human immunodeficiency virus]. / Synthèse de carbamoyl tétrahydro 1,4,2-dioxazines et evaluation de leur effet contre le virus de l'immunodéficience humaine.

1,4,2-dioxazine derivatives were synthesized from B-uréidoxyalcools, and their 1H, 13C RMN and mass spectra were determined. Their activity against human immunodeficiency virus and their cytotoxicity were then evaluated. Whereas the derivatives had no effect on virus infectivity nor on reverse transcriptase activity, they unexpectedly enhanced host cell infection by both lymphotropic and macrophage-tropic virus strains.

2-Acetyl-4H-benzothiazin-3(2H)-one.

The title compound, C(10)H(9)NO(2)S, has a boat-shaped heterocyclic six-membered ring such that the S and N atoms lie essentially in the plane of the benzene ring while the remaining two C atoms are above this plane.

Antibacterial and molluscicidal activities of the essential oil of Chrysanthemum viscidehirtum.

The volatile fraction of Chrysanthemum viscidehirtum aerial parts, consisting mainly of limonene, beta-farnesene and many oxygenated sesquiterpenes, was screened for activity against 21 microbial strains. This essential oil exhibited activity against all germs tested, in particular Salmonella typhi and Proteus mirabilis. It also showed molluscicidal activity against Bulinus truncatus.

[Synthesis and pharmacologic study of 1,5-dialkyl-1,5-benzodiazepine-2,4-dithiones]. / Synthèse et étude pharmacologique des 1,5-dialkyl-1,5-benzodiazépine-2,4-dithiones.

The synthesis and psychotropic activity of 1,5-diakyl-1,5-benzodiazepine-2,4-dithiones (alkyl = methyl, ethyl and benzyl radicals) were studied. Alkylation reactions were performed in catalytic conditions by phase transfer. These reactions allowed us to isolate only one kind of product N-alkyl. Acute toxicity studies were conducted according to European protocols in two species of appropriate mammals in order to discover the lethal doses. The activity of the compounds on the CNS was then studied, using a battery of compartmental tests used in psychopharmacology. No toxicity was demonstrated at therapeutic doses. Each product had a sedative effect more or less pronounced and different from the reference substance clobazam (Urbanyl). They also had myorelaxant and anxiolytic effects, even lengthening the hypnotic effect of thiopental (synergic action).

[Synthesis and pharmacologic study of 1,5-benzodiazepine-2,4-diones and their alkyl derivatives]. / Synthèse et étude pharmacologique des 1,5-benzodiazépine-2,4-diones et de leurs dérivés alkylés.

From the pharmacodynamic studies of 1,5-benzodiazepin-2,4-diones and alkyl derivatives prepared in our laboratories, we can conclude that these products are not toxic at therapeutic dosage. They have sedative, myorelaxant and anxiolytic actions. The two products alkylated by allyl bromide have also hypnotic, sedative and anticonvulsant properties.

[Synthesis and pharmacologic study of 1,5-benzodiazepine-2,4-dithiones and their alkyl derivatives]. / Synthèse et étude pharmacologique des 1,5-benzodiazépine-2,4-dithiones et de leurs dérivés alkylés.

From the pharmacodynamic studies of 1,5-benzodiazepine-2,4-dithiones and alkyl derivatives, we can conclude that these products are not toxic at therapeutic dosage. They have sedative, myorelaxant and anxiolytic actions.

Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents.

The synthesis and the antiviral activities of C-3 acyclic nucleoside analogues of imidazo[1,2-a]pyridine and pyrimidine are reported. From these compounds, 20, 21, 22, 23, 28, and 34 showed a specific activity against cytomegalovirus and/or varicella-zoster virus.